EEDi-5273

• CAT Number: I045332
• CAS Number: 2585648-55-9
• Molecular Formula: C26H22F4N6O2
• Molecular Weight: 526.49
• Purity: ≥95%
• Synonyms: 15-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]-9-propan-2-yl-5-(trifluoromethyl)-4,9,12,14,16-pentazatetracyclo[9.6.1.02,7.014,18]octadeca-1(17),2,4,6,11(18),12,15-heptaen-10-one
• InChI: InChI=1S/C26H22F4N6O2/c1-13(2)35-11-14-7-21(26(28,29)30)31-8-16(14)18-10-33-25(36-12-34-22(23(18)36)24(35)37)32-9-17-15-5-6-38-20(15)4-3-19(17)27/h3-4,7-8,10,12-13H,5-6,9,11H2,1-2H3,(H,32,33)
• InChIKey: OAYMRNSLBKYMKG-UHFFFAOYSA-N
• SMILES: CC(C)N1CC2=CC(=NC=C2C3=CN=C(N4C3=C(C1=O)N=C4)NCC5=C(C=CC6=C5CCO6)F)C(F)(F)F

EEDi‑5273 (Cat No.: I045332) is a highly potent, orally bioavailable small‑molecule inhibitor of the PRC2 component EED (Embryonic Ectoderm Development). It binds with an IC₅₀ around 0.2 nM, effectively inhibiting PRC2 methyltransferase activity and reducing H3K27me₃ levels in cells . In preclinical xenograft models (e.g. KARPAS‑422 lymphoma), oral dosing led to complete and durable tumor regression without toxicity. EEDi‑5273 is under active development for oncology and potentially non‑cancer indications such as hemoglobinopathies, as a next‑generation epigenetic modulator.

Reference

[1]. Rej RK, et al. Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression. J Med Chem. 2021 Oct 14;64(19):14540-14556.
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